Am. Alobaid et al., SYNTHESIS AND BIOLOGICAL EVALUATION OF NEW CYCLOPENTENO[B]THIOPHENE DERIVATIVES AS LOCAL-ANESTHETIC AND ANTIARRHYTHMIC AGENTS, Die Pharmazie, 53(1), 1998, pp. 24-28
A series of ethyl 2-subsituted amino-cyclopenteno[b]thiophen-3-carboxy
lates was synthesized as a carticaine analogues and evaluated for thei
r local anesthetic and antiarrhythmic activity. Compounds ethyl 2-[1-o
xo-2-(ethylamino)ethylamino]-(4a), ethyl 2-[1-oxo-2-(n-propylamino)-et
hylamino]-(4c), ethyl 2-[1-oxo-2-(4-methylpiperazino)ethylamino]-(4e),
ethyl 2-[1-oxo-2-(ethylamino)propylamino]-(5a) and ethyl )propylamino
]cyclopenteno[b]thiophen-3-carboxylate (5c) proved to possess local an
esthetic and antiarrhythmic activity comparable to carticaine and lido
caine, The active compounds exert their antiarrhythmic potency via blo
cking Na+ channels as in case of 5c or blocking Ca+2 channels as in ca
se of 4a, 4e and 5c. Compound 4e exhibited a dual mechanism by blockin
g both Na+ and Ca+2 channels.